1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. SNC80

SNC80  (Synonyms: NIH 10815)

目录号: HY-101202 纯度: 99.44%
COA 产品使用指南

SNC80 (NIH 10815) 是一种有效的,高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂,Ki 为1.78 nM,IC50 为 2.73 nM。SNC80 还以 EC50 为 52.8 nM 来选择性激活 HEK293 细胞中的 μ-δ 异聚体。SNC80 具有抗伤害性,抗痛觉过敏和抗抑郁样作用,并可用于多种头痛症的研究。

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SNC80 Chemical Structure

SNC80 Chemical Structure

CAS No. : 156727-74-1

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Other Forms of SNC80:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment[1][2][3][4][5][6].

IC50 & Target

IC50: 2.73 nM (δ-opioid receptor), 5457 nM (μ-opioid receptor)[3]
Ki: 1.78 nM (δ-opioid receptor), 881.5 nM (μ-opioid receptor) and 441.8 nM (κ-opioid receptor)[2]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
C6 EC50
166 nM
Compound: SNC-80
Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay
Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay
[PMID: 19788201]
CHO EC50
14.4 nM
Compound: SNC80
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
[PMID: 31834798]
CHO EC50
15.7 nM
Compound: SNC-80
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 19362480]
CHO EC50
210 nM
Compound: SNC80
Agonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
[PMID: 30996778]
CHO ED50
26 nM
Compound: SNC-80
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
[PMID: 17625813]
CHO EC50
4.8 nM
Compound: SNC 80
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
[PMID: 23142613]
CHO EC50
4.8 nM
Compound: SNC-80
Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
[PMID: 17935988]
CHO EC50
7.6 nM
Compound: SNC80
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
[PMID: 32435376]
HEK293 EC50
0.14 nM
Compound: SNC80
Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method
Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method
[PMID: 24900842]
HEK293 IC50
0.8 nM
Compound: SNC-80
Displacement of [3H]DPDPE from mouse delta opioid receptor expressed in HEK293 cells by liquid scintillation counting
Displacement of [3H]DPDPE from mouse delta opioid receptor expressed in HEK293 cells by liquid scintillation counting
[PMID: 19646882]
HEK293 EC50
1.7 nM
Compound: SNC80
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
[PMID: 24900842]
HEK293 EC50
15.7 nM
Compound: SNC80
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
[PMID: 22197670]
HEK293 IC50
3601 nM
Compound: SNC-80
Displacement of [3H]U69593 from rat kappa opioid receptor expressed in HEK293 cells by liquid scintillation counting
Displacement of [3H]U69593 from rat kappa opioid receptor expressed in HEK293 cells by liquid scintillation counting
[PMID: 19646882]
HEK293 EC50
5264 nM
Compound: SNC80
Agonist activity at human kappa opioid receptor expressed in HEK293 cells by CellKey method
Agonist activity at human kappa opioid receptor expressed in HEK293 cells by CellKey method
[PMID: 24900842]
HEK293 IC50
6066 nM
Compound: SNC-80
Displacement of [3H]DAMGO from mouse mu opioid receptor expressed in HEK293 cells by liquid scintillation counting
Displacement of [3H]DAMGO from mouse mu opioid receptor expressed in HEK293 cells by liquid scintillation counting
[PMID: 19646882]
体外研究
(In Vitro)

SNC80 selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 exhibits substantially greater activity in cells coexpressing μ- and δ-opioid receptors than in cells either singly expressing δ-opioid receptors or coexpressing δ- and κ-opioid receptors[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SNC80 (10 mg/kg; intraperitoneal injection; once; C57BL6/J mice) treatment significantly attenuated this allodynia caused by overuse of Sumatriptan[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female C57BL6/J mice (20-30g) injected with Sumatriptan[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; once
Result: Significantly attenuated allodynia.
分子量

449.63

Formula

C28H39N3O2

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 33.33 mg/mL (74.13 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈3); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2241 mL 11.1203 mL 22.2405 mL
5 mM 0.4448 mL 2.2241 mL 4.4481 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.33 mg/mL (7.41 mM); 澄清溶液

    此方案可获得 ≥ 3.33 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.33 mg/mL (7.41 mM); 澄清溶液

    此方案可获得 ≥ 3.33 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2241 mL 11.1203 mL 22.2405 mL 55.6013 mL
5 mM 0.4448 mL 2.2241 mL 4.4481 mL 11.1203 mL
10 mM 0.2224 mL 1.1120 mL 2.2241 mL 5.5601 mL
15 mM 0.1483 mL 0.7414 mL 1.4827 mL 3.7068 mL
20 mM 0.1112 mL 0.5560 mL 1.1120 mL 2.7801 mL
25 mM 0.0890 mL 0.4448 mL 0.8896 mL 2.2241 mL
30 mM 0.0741 mL 0.3707 mL 0.7414 mL 1.8534 mL
40 mM 0.0556 mL 0.2780 mL 0.5560 mL 1.3900 mL
50 mM 0.0445 mL 0.2224 mL 0.4448 mL 1.1120 mL
60 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9267 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SNC80
目录号:
HY-101202
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